MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors

The Aurora kinases are essential for cell mitosis, and the dysregulation of Aurora A and B have been linked to the etiology of human cancers. Investigational agents MLN8054 (<b>8</b>) and alisertib (MLN8237, <b>10</b>) have been identified as high affinity, selective, orally bioavailable inhibitors of Aurora A that have advanced into human clinical trials. Alisertib (<b>10</b>) is currently being evaluated in multiple Phase II and III clinical trials in hematological malignancies and solid tumors